WO2017139664A8 - Intermediates in the synthesis of eribulin and related methods of synthesis - Google Patents

Intermediates in the synthesis of eribulin and related methods of synthesis Download PDF

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Publication number
WO2017139664A8
WO2017139664A8 PCT/US2017/017501 US2017017501W WO2017139664A8 WO 2017139664 A8 WO2017139664 A8 WO 2017139664A8 US 2017017501 W US2017017501 W US 2017017501W WO 2017139664 A8 WO2017139664 A8 WO 2017139664A8
Authority
WO
WIPO (PCT)
Prior art keywords
synthesis
eribulin
intermediates
related methods
methods
Prior art date
Application number
PCT/US2017/017501
Other languages
French (fr)
Other versions
WO2017139664A1 (en
Inventor
Phil S. Baran
Charles E. Chase
Francis G. Fang
Original Assignee
Eisai R&D Management Co., Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Eisai R&D Management Co., Ltd. filed Critical Eisai R&D Management Co., Ltd.
Priority to JP2018539136A priority Critical patent/JP6786610B2/en
Priority to RU2018132264A priority patent/RU2732575C2/en
Priority to SG11201806133UA priority patent/SG11201806133UA/en
Priority to MX2018009794A priority patent/MX2018009794A/en
Priority to US16/076,028 priority patent/US10676481B2/en
Priority to KR1020187025945A priority patent/KR20180107243A/en
Priority to EP17750887.6A priority patent/EP3413887B1/en
Priority to CN201780010903.XA priority patent/CN108601760A/en
Publication of WO2017139664A1 publication Critical patent/WO2017139664A1/en
Priority to IL260717A priority patent/IL260717B/en
Publication of WO2017139664A8 publication Critical patent/WO2017139664A8/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/22—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis

Abstract

The invention relates to methods and intermediates useful in the synthesis of eribulin.
PCT/US2017/017501 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis WO2017139664A1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
JP2018539136A JP6786610B2 (en) 2016-02-12 2017-02-10 Intermediates and related synthetic methods in the synthesis of eribulin
RU2018132264A RU2732575C2 (en) 2016-02-12 2017-02-10 Intermediate products in synthesis of eribulin and corresponding methods of synthesis
SG11201806133UA SG11201806133UA (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis
MX2018009794A MX2018009794A (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis.
US16/076,028 US10676481B2 (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis
KR1020187025945A KR20180107243A (en) 2016-02-12 2017-02-10 Intermediates and related synthetic methods in the synthesis of eribulin
EP17750887.6A EP3413887B1 (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis
CN201780010903.XA CN108601760A (en) 2016-02-12 2017-02-10 Intermediate in the synthesis of eribulin and relevant synthetic method
IL260717A IL260717B (en) 2016-02-12 2018-07-22 Intermediates in the synthesis of eribulin and related methods of synthesis

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662294538P 2016-02-12 2016-02-12
US62/294,538 2016-02-12

Publications (2)

Publication Number Publication Date
WO2017139664A1 WO2017139664A1 (en) 2017-08-17
WO2017139664A8 true WO2017139664A8 (en) 2018-07-26

Family

ID=59563582

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/017501 WO2017139664A1 (en) 2016-02-12 2017-02-10 Intermediates in the synthesis of eribulin and related methods of synthesis

Country Status (10)

Country Link
US (1) US10676481B2 (en)
EP (1) EP3413887B1 (en)
JP (1) JP6786610B2 (en)
KR (1) KR20180107243A (en)
CN (1) CN108601760A (en)
IL (1) IL260717B (en)
MX (1) MX2018009794A (en)
RU (1) RU2732575C2 (en)
SG (1) SG11201806133UA (en)
WO (1) WO2017139664A1 (en)

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JP5735277B2 (en) 2007-10-03 2015-06-17 エーザイ・アール・アンド・ディー・マネジメント株式会社 Intermediates and methods for the synthesis of halichondrin B analogues
US8203010B2 (en) 2010-01-26 2012-06-19 Eisai R&D Management Co., Ltd. Compounds useful in the synthesis of halichondrin B analogs
CN114716453A (en) 2013-11-04 2022-07-08 卫材R&D管理有限公司 Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B
US9303039B2 (en) 2013-12-06 2016-04-05 Eisai R&D Management Co., Ltd. Methods useful in the synthesis of halichondrin B analogs
MX2017014237A (en) 2015-05-07 2018-09-17 Eisai R&D Man Co Ltd Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides.
EP3478691A4 (en) 2016-06-30 2020-07-22 Eisai R&D Management Co., Ltd. Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof
CN111868044A (en) 2018-01-03 2020-10-30 卫材R&D管理有限公司 Prins reaction and compounds useful for the synthesis of halichondrin macrolides and analogs thereof
CN110568121A (en) * 2019-07-11 2019-12-13 山东省药学科学院 Eribulin and detection method of related substances in eribulin-containing preparation

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US5338865A (en) 1992-03-12 1994-08-16 President And Fellows Of Harvard College Synthesis of halichondrin B and norhalichondrin B
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CN114716453A (en) 2013-11-04 2022-07-08 卫材R&D管理有限公司 Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B
US9303039B2 (en) 2013-12-06 2016-04-05 Eisai R&D Management Co., Ltd. Methods useful in the synthesis of halichondrin B analogs
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MX2017014237A (en) 2015-05-07 2018-09-17 Eisai R&D Man Co Ltd Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides.
EP3478691A4 (en) 2016-06-30 2020-07-22 Eisai R&D Management Co., Ltd. Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof
WO2018217894A1 (en) 2017-05-24 2018-11-29 Eisai R&D Management Co., Ltd. Fluorine-labelled halichondrin derivatives and related methods of synthesis
CN111868044A (en) 2018-01-03 2020-10-30 卫材R&D管理有限公司 Prins reaction and compounds useful for the synthesis of halichondrin macrolides and analogs thereof

Also Published As

Publication number Publication date
RU2732575C2 (en) 2020-09-21
US20190300542A1 (en) 2019-10-03
MX2018009794A (en) 2018-12-17
US10676481B2 (en) 2020-06-09
RU2018132264A3 (en) 2020-04-15
EP3413887A1 (en) 2018-12-19
JP2019504839A (en) 2019-02-21
EP3413887A4 (en) 2019-08-14
WO2017139664A1 (en) 2017-08-17
EP3413887B1 (en) 2021-04-07
CN108601760A (en) 2018-09-28
RU2018132264A (en) 2020-03-12
JP6786610B2 (en) 2020-11-18
IL260717B (en) 2020-10-29
SG11201806133UA (en) 2018-08-30
KR20180107243A (en) 2018-10-01

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